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CYT387, a Novel JAK2 Inhibitor, Suppresses IL-13-Induced Epidermal Barrier Dysfunction Via miR-143 Targeting IL-13Ralpha1 and STAT3.
Zu Y, Chen XF, Li Q, Zhang ST. Zu Y, et al. Biochem Genet. 2020 Nov 15. doi: 10.1007/s10528-020-10003-0. Online ahead of print. Biochem Genet. 2020. PMID: 33190168
It is well-known that AD has a complex pathogenesis without effective therapy. Herein, we explored the function and mechanism of CYT387, a novel JAK2 inhibitor, on epidermal barrier damage. HaCaT cells exposed with high-concentration Ca(2+) (1.8 mM) for 14 days were …
It is well-known that AD has a complex pathogenesis without effective therapy. Herein, we explored the function and mechanism of CYT387 …
JAK1/2 Inhibitors AZD1480 and CYT387 Inhibit Canine B-Cell Lymphoma Growth by Increasing Apoptosis and Disrupting Cell Proliferation.
Lu Z, Hong CC, Jark PC, Assumpção ALFV, Bollig N, Kong G, Pan X. Lu Z, et al. J Vet Intern Med. 2017 Nov;31(6):1804-1815. doi: 10.1111/jvim.14837. Epub 2017 Sep 27. J Vet Intern Med. 2017. PMID: 28960447 Free PMC article.
The Janus kinase (JAK) and signal transducer and activator of transcription (STAT) pathways play important roles in the pathogenesis of hematologic malignancies in humans including DLBCLs. AZD1480 and CYT387 are novel JAK1/2 inhibitors that have been used in clinica …
The Janus kinase (JAK) and signal transducer and activator of transcription (STAT) pathways play important roles in the pathogenesis of hema …
Drug repositioning of TANK-binding kinase 1 inhibitor CYT387 as an alternative for the treatment of Gram-negative bacterial sepsis.
Lee SJ, Gharbi A, You JS, Han HD, Kang TH, Hong SH, Park WS, Jung ID, Park YM. Lee SJ, et al. Int Immunopharmacol. 2019 Aug;73:482-490. doi: 10.1016/j.intimp.2019.05.051. Epub 2019 Jun 4. Int Immunopharmacol. 2019. PMID: 31173970
CYT387 also inhibited pro-inflammatory cytokine and surface molecule expression by mature DCs after LPS exposure. ...In conclusion, our study suggests that drug repositioning of CYT387 may serve as a potential therapeutic for sepsis....
CYT387 also inhibited pro-inflammatory cytokine and surface molecule expression by mature DCs after LPS exposure. ...In conclusion, o …
CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms.
Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, Loriaux MM, Druker BJ, Burns CJ, Fantino E, Deininger MW. Tyner JW, et al. Blood. 2010 Jun 24;115(25):5232-40. doi: 10.1182/blood-2009-05-223727. Epub 2010 Apr 12. Blood. 2010. PMID: 20385788 Free PMC article.
We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1, JAK2, and tyrosine kinase 2 (TYK2) at low nanomolar concentrations, with few additional targets. ...In a murine MPN model, CYT387 normalized white cell counts, hematocrit, spleen …
We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1, JAK2, and tyrosine kinase 2 (TYK2) at low nano …
In Vivo Modeling of Chemoresistant Neuroblastoma Provides New Insights into Chemorefractory Disease and Metastasis.
Yogev O, Almeida GS, Barker KT, George SL, Kwok C, Campbell J, Zarowiecki M, Kleftogiannis D, Smith LM, Hallsworth A, Berry P, Möcklinghoff T, Webber HT, Danielson LS, Buttery B, Calton EA, da Costa BM, Poon E, Jamin Y, Lise S, Veal GJ, Sebire N, Robinson SP, Anderson J, Chesler L. Yogev O, et al. Cancer Res. 2019 Oct 15;79(20):5382-5393. doi: 10.1158/0008-5472.CAN-18-2759. Epub 2019 Aug 12. Cancer Res. 2019. PMID: 31405846 Free article.
The antiapoptotic, prometastatic JAK-STAT3 pathway was activated in chemoresistant tumors, and treatment with the JAK1/JAK2 inhibitor CYT387 reduced progression of chemoresistant tumors and increased survival. ...SIGNIFICANCE: An in vivo mouse model of high-risk treatment- …
The antiapoptotic, prometastatic JAK-STAT3 pathway was activated in chemoresistant tumors, and treatment with the JAK1/JAK2 inhibitor CYT …
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, Tefferi A. Pardanani A, et al. Leukemia. 2009 Aug;23(8):1441-5. doi: 10.1038/leu.2009.50. Epub 2009 Mar 19. Leukemia. 2009. PMID: 19295546
CYT387 is an ATP-competitive small molecule that potently inhibits JAK1/JAK2 kinases (IC(50)=11 and 18 nM, respectively), with significantly less activity against other kinases, including JAK3 (IC(50)=155 nM). ...Overall, our data indicate that the JAK1/JAK2 selective inhi …
CYT387 is an ATP-competitive small molecule that potently inhibits JAK1/JAK2 kinases (IC(50)=11 and 18 nM, respectively), with signif …
Safety and efficacy of CYT387, a JAK1 and JAK2 inhibitor, in myelofibrosis.
Pardanani A, Laborde RR, Lasho TL, Finke C, Begna K, Al-Kali A, Hogan WJ, Litzow MR, Leontovich A, Kowalski M, Tefferi A. Pardanani A, et al. Leukemia. 2013 Jun;27(6):1322-7. doi: 10.1038/leu.2013.71. Epub 2013 Mar 5. Leukemia. 2013. PMID: 23459451 Free PMC article.
JAK-STAT is a rational drug target in myelofibrosis (MF) given its association with JAK2/MPL mutations and aberrant inflammatory cytokine expression. We conducted a Phase 1/2 trial of CYT387, a potent JAK1/2 inhibitor, in patients with high- or intermediate-r …
JAK-STAT is a rational drug target in myelofibrosis (MF) given its association with JAK2/MPL mutations and aberrant inflammatory cytokine ex …
P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387.
Durmus S, Xu N, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH. Durmus S, et al. Pharmacol Res. 2013 Oct;76:9-16. doi: 10.1016/j.phrs.2013.06.009. Epub 2013 Jul 1. Pharmacol Res. 2013. PMID: 23827160
CYT387 is an orally bioavailable, small molecule inhibitor of Janus family of tyrosine kinases (JAK) 1 and 2. ...Despite the similar systemic exposure, brain accumulation of CYT387 was increased 10.5- and 56-fold in the Bcrp1;Mdr1a/1b(-/-) mice compared to th …
CYT387 is an orally bioavailable, small molecule inhibitor of Janus family of tyrosine kinases (JAK) 1 and 2. ...Despite the s …
The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells.
Monaghan KA, Khong T, Burns CJ, Spencer A. Monaghan KA, et al. Leukemia. 2011 Dec;25(12):1891-9. doi: 10.1038/leu.2011.175. Epub 2011 Jul 26. Leukemia. 2011. PMID: 21788946
JAKs therefore make a rational drug target for anti-MM therapy. CYT387 is a novel, orally bioavailable JAK1/2 inhibitor, which has recently been described. ...Cell cycling was inhibited with a G(2)/M accumulation of cells, and apoptosis was induced by CYT3 …
JAKs therefore make a rational drug target for anti-MM therapy. CYT387 is a novel, orally bioavailable JAK1/2 inhibitor, which …
Enhanced Antitumor Activity of Cetuximab in Combination with the Jak Inhibitor CYT387 against Non-Small-Cell Lung Cancer with Various Genotypes.
Hu Y, Dong XZ, Liu X, Liu P, Chen YB. Hu Y, et al. Mol Pharm. 2016 Feb 1;13(2):689-97. doi: 10.1021/acs.molpharmaceut.5b00927. Epub 2015 Dec 29. Mol Pharm. 2016. PMID: 26685983
However, resistance to EGFR inhibitors limits its effectiveness. In this study, we investigated the effectiveness of Jak-2 inhibitor, CYT387, in combination with cetuximab. Xenograft animal models were administered with cetuximab or CYT387 or their combinatio …
However, resistance to EGFR inhibitors limits its effectiveness. In this study, we investigated the effectiveness of Jak-2 inhibitor, …
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